Nanotechnology has provided many promising nanoplatforms for targeted cancer imaging and therapy. Among these platforms, gold nanoparticles (GNPs) play a unique role in medicine because of their excellent physical and chemical properties. To expand the applications of GNPs in medicine, amounts of targeting moieties, imaging labels, and therapeutic agents have been integrated into these particles to form multifunctionalized GNPs. In this review, we highlight recent advances of the fabrication of cancer-targeting multifunctionalized GNPs and their applications in imaging and therapy.; Nanotechnology has provided many promising nanoplatforms for targeted cancer imaging and therapy. Among these platforms, gold nanoparticles (GNPs) play a unique role in medicine because of their excellent physical and chemical properties. To expand the applications of GNPs in medicine, amounts of targeting moieties, imaging labels, and therapeutic agents have been integrated into these particles to form multifunctionalized GNPs. In this review, we highlight recent advances of the fabrication of cancer-targeting multifunctionalized GNPs and their applications in imaging and therapy.